The effects on ileal contraction of some synthetic derivatives of the bioactive [1–3] 3,4-secoisopimara-4(18),7,15-trien-3-oic acid (1) isolated from S. cinnabarina are reported.Strips of guinea pig ileum (GPI) were suspended in an organ bath and a resting tension of 1g was applied. Contractile responses were recorded isotonically and expressed as percentage of maximal responses of acetylcholine (Ach, 10−6M, contact time 30 sec). The strips were treated with increasing non-cumulative concentrations of 1 derivatives (10−7–10−4 M, contact time 30 min before Ach). These compounds induced a dose-dependent reduction of the contractile activity of Ach, with the following decreasing order of IC50: 6 (1x10−5M) > 4 (1.9x10−5M) > 7 (3.3x10−5M) = 9 (3.5x10−5M) > 1 (4.2x10−5M) > 3 (5.2x10−5M) = 5 (5.8x10−5M) = 2 (6x10−5M) = 10 (6x10−5M).
Antispasmodic Activity of Semi-Synthetic Secoisopimarane Derivatives.
BRUNO, OLGA;BISIO, ANGELA
2009-01-01
Abstract
The effects on ileal contraction of some synthetic derivatives of the bioactive [1–3] 3,4-secoisopimara-4(18),7,15-trien-3-oic acid (1) isolated from S. cinnabarina are reported.Strips of guinea pig ileum (GPI) were suspended in an organ bath and a resting tension of 1g was applied. Contractile responses were recorded isotonically and expressed as percentage of maximal responses of acetylcholine (Ach, 10−6M, contact time 30 sec). The strips were treated with increasing non-cumulative concentrations of 1 derivatives (10−7–10−4 M, contact time 30 min before Ach). These compounds induced a dose-dependent reduction of the contractile activity of Ach, with the following decreasing order of IC50: 6 (1x10−5M) > 4 (1.9x10−5M) > 7 (3.3x10−5M) = 9 (3.5x10−5M) > 1 (4.2x10−5M) > 3 (5.2x10−5M) = 5 (5.8x10−5M) = 2 (6x10−5M) = 10 (6x10−5M).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.